Pirenzepine

Modify Date: 2026-06-30 20:09:25

Pirenzepine structure	Common Name	Pirenzepine
	CAS Number	28797-61-7	Molecular Weight	351.402
	Density	1.3±0.1 g/cm3	Boiling Point	541.7±50.0 °C at 760 mmHg
	Molecular Formula	C₁₉H₂₃Cl₂N₅O₂	Melting Point	226 - 230ºC
	MSDS	N/A	Flash Point	281.4±30.1 °C

Use of Pirenzepine

Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].

Name	pirenzepine
Synonym	More Synonyms

Description	Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Neuronal Signaling >> mAChR Signaling Pathways >> GPCR/G Protein >> mAChR Research Areas >> Metabolic Disease
In Vitro	Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity[2]. Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration[2]. Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells[2]. Cell Proliferation Assay[2] Cell Line: PC-3 cells Concentration: 100-140 μg/mL Incubation Time: 24 hours Result: Inhibited PC-3 cell proliferation in a concentration-dependent manner. Cell Migration Assay [2] Cell Line: PC-3 and A549 cells Concentration: 110 μg/mL Incubation Time: 24 hours Result: Inhibited the migration of PC-3 and A549 cell lines (P=0.014). Western Blot Analysis[2] Cell Line: PC-3 cells Concentration: 110 μg/mL Incubation Time: 0-24 hours Result: Inhibited the expression of GLI1 and PTCH1. RT-PCR[2] Cell Line: PC-3 cell Concentration: 100-130 μg/mL Incubation Time: 24 hours Result: Suppressed GLI1 mRNA expression in PC-3 cells. Increased PTCH1 mRNA level but not reach statistical significance. Showed no SHH mRNA expression level change.
In Vivo	Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock[3]. Animal Model: Male C57BL/6 mice with experimental endotoxemia[3] Dosage: 0.3 mg/kg Administration: Intraperitoneal injection; 0.3 mg/kg; once Result: Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.

Density	1.3±0.1 g/cm3
Boiling Point	541.7±50.0 °C at 760 mmHg
Melting Point	226 - 230ºC
Molecular Formula	C₁₉H₂₃Cl₂N₅O₂
Molecular Weight	351.402
Flash Point	281.4±30.1 °C
Exact Mass	351.169525
PSA	74.23000
LogP	-0.08
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.615
InChIKey	RMHMFHUVIITRHF-UHFFFAOYSA-N
SMILES	CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1
Storage condition	Store at RT

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UU7882950

CHEMICAL NAME :: 6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-

CAS REGISTRY NUMBER :: 28797-61-7

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H21-N5-O2

MOLECULAR WEIGHT :: 351.45

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3046 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 427 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 156 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

Precursor 10
CAS#:84446-20-8 11-[2-(4-methyl... CAS#:956-30-9 2-Amino-N-(2-ch... CAS#:885-70-1 5,6-Dihydro-6-o... CAS#:84446-21-9 3-(2'-chloroben...
CAS#:109-01-3 methylpiperazine CAS#:84446-18-4 1-oxo-5,11-dihy... CAS#:84446-17-3 3-(2'-bromobenz... CAS#:88369-72-6 2-amino-N-(2-ch...
CAS#:84446-16-2 2-chloro-N-(2-c... CAS#:84446-15-1 2-bromo-N-(2-ch...
DownStream 0

Name: Ratio IC50 values of Muscarinic M3 receptor and muscarinic M1 receptor
Source: ChEMBL
Target: Muscarinic acetylcholine receptor M1 and M3
External Id: CHEMBL881261

Name: Ratio IC50 values of Muscarinic M2 receptor and muscarinic M1 receptor
Source: ChEMBL
Target: Muscarinic acetylcholine receptors; M1 & M2
External Id: CHEMBL841069

Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase

Name: Cytochrome P450 Family 1 Subfamily A Member 2 (CYP1A2) small molecule antagonists: lu...
Source: 824
External Id: CYP273

Name: Partition coefficient (logD6.5)
Source: ChEMBL
Target: N/A
External Id: CHEMBL646647

Name: Confirmatory qHTS assay for inhibitors of human arachidonate 12S-lipoxygenase (ALOX12...
Source: NCGC
External Id: 12hLO-f-round2

Name: Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured a...
Source: ChEMBL
Target: Musca domestica
External Id: CHEMBL3061007

Name: Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured a...
Source: ChEMBL
Target: Musca domestica
External Id: CHEMBL3061008

Name: Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured a...
Source: ChEMBL
Target: Musca domestica
External Id: CHEMBL3061009

Name: Increase the activity of the Burkholderia fixLJ 2-component system
Source: ICCB-Longwood/NSRB Screening Facility, Harvard Medical School
Target: Burkholderia multivorans
External Id: HMS1625

Total 530, Current Page 1 of 53

Piclamilast

11-[(4-Methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one

Cpodpmb

11-[(4-Methyl-1-piperazinyl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one

Pirenzepine

Gastrozepin

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HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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Precursor & DownStream

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Synonyms

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.